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Assay Detail

CHEMBL4729467

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of polymer supported probe 25 binding to IRAK4 in human THP-1 cell lysates preincubated for 45 mins under shaking condition followed by probe addition and measured after 30 mins by mass spectrometry based chemoproteomic analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Subcellular Lysates
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Interleukin-1 receptor-associated kinase 4 (CHEMBL3778)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase.
Degorce SL,Tavana O,Banks E,Crafter C,Gingipalli L,Kouvchinov D,Mao Y,Pachl F,Solanki A,Valge-Archer V,Yang B,Edmondson SD
J Med Chem (2020) 63 : 10460 -10473
PubMed 32803978 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 5.44 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4749646 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4749646 Kd = 3600.0 nM 5.44